MIP-1375

**MIP-1375** is a small-molecule inhibitor of prostate-specific membrane antigen (PSMA), designed for radiolabeling with iodine-131 ([^131^I]MIP-1375) as a targeted radiopharmaceutical for prostate cancer therapy. Developed initially by Molecular Insight Pharmaceuticals (later acquired by Progenics Pharmaceuticals and Lantheus Holdings), it demonstrated preclinical efficacy in inhibiting tumor growth in LNCaP xenograft models in a time- and dose-dependent manner at clinically relevant radioactivity doses. It enables high tumor uptake with potential for treating metastatic castration-resistant prostate cancer (mCRPC), though human clinical data appear limited compared to related analogs like MIP-1095/1466.